glioma and glioblastoma

By Targets:	Apoptosis (4) Autophagy (2) c-Myc (1) Endogenous Metabolite (1) ERK (1) Histone Methyltransferase (1) HIV (1) JNK (1) mTOR (1) NF-κB (2) P2X Receptor (1) p38 MAPK (1) Peptide-Drug Conjugates (PDCs) (1) Pyruvate Kinase (1) Reactive Oxygen Species (ROS) (1) Reverse Transcriptase (1) ROCK (1) SGK (1) WDR5 (1)
By Research Areas:	Cancer (9) Infection (1) Inflammation/Immunology (2) Neurological Disease (2)

Targets Recommended: Fat Mass and Obesity-associated Protein (FTO)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-124582

NEO214 1 Publications Verification	Autophagy mTOR	Cancer
NEO214 is an autophagy inhibitor and a covalent conjugate of the PDE4 inhibitor Rolipram (HY-16900) and perillyl alcohol (HY-N7000). It has anti-cancer activity and blood-brain barrier (BBB) permeability. Over sex. NEO214 prevents autophagy-lysosome fusion, thereby blocking autophagic flux and triggering glioma cell death. The process involves mTOR activation, andTFEB(Transcription Factor EB) aggregation. NEO214 inhibitionMacroautophagy/autophagy in glioblastoma cells has the potential to overcome chemotherapy resistance in glioblastoma .

HY-N5025

Bullatine A	P2X Receptor Apoptosis ERK p38 MAPK c-Myc NF-κB Reactive Oxygen Species (ROS)	Neurological Disease Inflammation/Immunology Cancer
Bullatine A, a diterpenoid alkaloid, is a potent P2X7 antagonist. Bullatine A possesses anti-rheumatic, anti-inflammatory and anti-nociceptive effects. Bullatine A inhibits ATP-induced BV-2 cell death/apoptosis and P2X receptor-mediated inflammatory responses. Bullatine A suppresses glioma cell growth by targeting SIRT6. Bullatine A specifically attenuates pain hypersensitivity in rats. Bullatine A attenuates LPS (HY-D1056)-induced systemic inflammatory response by inhibiting the ROS/JNK/NF-κB pathway in mice. Bullatine A improves despair behavior in Chronic chronic social defeat stress (CSDS) mice. Bullatine A can be used for the study of inflammation, glioblastoma (GBM) and depression .

HY-167832

PT109	JNK SGK ROCK	Neurological Disease Inflammation/Immunology Cancer
PT109 is a multi-kinase inhibitor. PT109 inhibits JNK (JNK1: IC₅₀=0.143 μM; JNK2: IC₅₀=0.831 μM; JNK3: IC₅₀=0.285 μM) and other kinases (SGK1: IC₅₀=1.34 μM; SGK2: IC₅₀=5.6 μM; SGK3: IC₅₀=26.4 μM; ROCK2: IC₅₀=34 μM) and plays an important role in anti-inflammation, anti-oxidation, neurogenesis, synaptogenesis, etc. In addition, PT109 also reprograms glioblastoma multiforme (GBM) into oligodendrocytes through the PTBP1/PKM1/2 pathway and changes the metabolic pattern of GBM, exerting anti-glioma activity .

HY-175802

HBI-2375 HYBI-084	WDR5 Histone Methyltransferase	Cancer
HBI-2375 (HYBI-084) is a selective, brain-penetrant and orally active MLL1-WDR5 interaction inhibitor. HBI-2375 inhibits WDR5 with an IC₅₀ of 4.48 nM. HBI-2375 shows inhibition of proliferation in MV4;11 leukemia cells (IC₅₀: 3.17 µM). HBI-2375 is capable of targeted disruption of histone methyltransferase activity in cancer cells. HBI-2375 can be used for the study of leukemia, glioma and glioblastoma .

HY-P10782

Pt(IV)-M13	Peptide-Drug Conjugates (PDCs)	Cancer
Pt(IV)-M13 is a BBB-penetrable Platinum (IV) prodrug-perfluoroaryl macrocyclic peptide conjugate. Pt(IV)-M13 is cytotoxic to glioma stem cells and increases uptake of platinum in the brain. Pt(IV)-M13 can be used in the study of glioblastoma .

HY-14266A

Dapivirine hydrochloride	Apoptosis Reverse Transcriptase Autophagy HIV	Infection
Dapivirine hydrochloride is a non-nucleoside reverse transcriptase inhibitor with antitumor activity. Dapivirine hydrochloride attenuates the proliferation of glioblastoma cells and induces apoptosis. Dapivirine hydrochloride modulates autophagy and activates Akt, Bad, and SAPK/JNK signaling pathways. Dapivirine hydrochloride has shown inhibitory effects on glioma cell growth both in vitro and in vivo. Dapivirine hydrochloride is also a promising drug candidate for topical microbial agents for the prevention of sexual transmission of HIV-1 .

HY-170577

PKM2-IN-8	Pyruvate Kinase Apoptosis	Cancer
PKM2-IN-8 (Compound 9b) is a pyruvate kinase M2 (PKM2) inhibitor (IC₅₀ = 0.31 μM). PKM2-IN-8 has potent antiproliferative activity against U87MG glioma cells. PKM2-IN-8 can induce early apoptosis and reduce lactate levels. PKM2-IN-8 can be used for the research of glioblastoma .

HY-149696

IR-Crizotinib	NF-κB	Cancer
IR-Crizotinib is a NF-κB-inducing kinase (NIK) inhibitor that crosses the blood-brain barrier and fluorescently localizes intracranial glioblastoma (GBM) in mice (IC₅₀=3.381 μM). IR-Crizotinib is conjugated from the near-infrared dye IR-786 and the NF-κB-inducing kinase (NIK) inhibitor Crizotinib. IR-Crizotinib can effectively inhibit the growth and invasion of glioma in vitro and in vivo and can be used in cancer research .

HY-174212

MXC-017	Apoptosis	Cancer
MXC-017 is a blood-brain barrier (BBB)-penetrant apoptosis inducer that directly targets Vimentin (VIM). MXC-017 prevents radiation-induced glioma stem cell (GSC) formation, while promoting G0/G1 cell cycle arrest and apoptosis. MXC-017 exhibits minimal off-target effects and shows no significant cytotoxicity. MXC-017 significantly prolongs median survival when used in combination with radiation therapy in glioblastoma (GBM) mouse models.

HY-W747597

Ganglioside GD1b Disodium Salt (Bovine Brain) Disialoganglioside GD1b; Ganglioside C1; Ganglioside G2	Endogenous Metabolite	Cancer
Ganglioside GD1b Disodium Salt (Bovine Brain) (Disialoganglioside GD1b; Ganglioside C1) is an acidic glycosphingolipid containing two sialic acid residues linked to an internal galactose unit. Ganglioside GD1b Disodium Salt tightly packs with cholesterol to form lipid microdomains that modulate intracellular and intercellular signaling events. Concentrations of Ganglioside GD1b Disodium Salt (Bovine Brain) in the human brain increase with age and are positively correlated with pilocytic astrocytoma tumor grade. Ganglioside GD1b Disodium Salt has been detected in various other gliomas, including primitive neuroectodermal tumors, glioblastomas, and anaplastic astrocytomas.

Cat. No.	Product Name	Type

HY-149696

IR-Crizotinib	Dyes
IR-Crizotinib is a NF-κB-inducing kinase (NIK) inhibitor that crosses the blood-brain barrier and fluorescently localizes intracranial glioblastoma (GBM) in mice (IC₅₀=3.381 μM). IR-Crizotinib is conjugated from the near-infrared dye IR-786 and the NF-κB-inducing kinase (NIK) inhibitor Crizotinib. IR-Crizotinib can effectively inhibit the growth and invasion of glioma in vitro and in vivo and can be used in cancer research .

IR-Crizotinib

Dyes

IR-Crizotinib is a NF-κB-inducing kinase (NIK) inhibitor that crosses the blood-brain barrier and fluorescently localizes intracranial glioblastoma (GBM) in mice (IC₅₀=3.381 μM). IR-Crizotinib is conjugated from the near-infrared dye IR-786 and the NF-κB-inducing kinase (NIK) inhibitor Crizotinib. IR-Crizotinib can effectively inhibit the growth and invasion of glioma in vitro and in vivo and can be used in cancer research .

Cat. No.	Product Name	Target	Research Area

HY-P10782

Pt(IV)-M13	Peptide-Drug Conjugates (PDCs)	Cancer
Pt(IV)-M13 is a BBB-penetrable Platinum (IV) prodrug-perfluoroaryl macrocyclic peptide conjugate. Pt(IV)-M13 is cytotoxic to glioma stem cells and increases uptake of platinum in the brain. Pt(IV)-M13 can be used in the study of glioblastoma .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N5025

Bullatine A	Alkaloids Piperidine Alkaloids Structural Classification Classification of Application Fields Ranunculaceae Source classification Aconitum carmichaeli Debx. Plants Inflammation/Immunology Disease Research Fields	P2X Receptor Apoptosis ERK p38 MAPK c-Myc NF-κB Reactive Oxygen Species (ROS)
Bullatine A, a diterpenoid alkaloid, is a potent P2X7 antagonist. Bullatine A possesses anti-rheumatic, anti-inflammatory and anti-nociceptive effects. Bullatine A inhibits ATP-induced BV-2 cell death/apoptosis and P2X receptor-mediated inflammatory responses. Bullatine A suppresses glioma cell growth by targeting SIRT6. Bullatine A specifically attenuates pain hypersensitivity in rats. Bullatine A attenuates LPS (HY-D1056)-induced systemic inflammatory response by inhibiting the ROS/JNK/NF-κB pathway in mice. Bullatine A improves despair behavior in Chronic chronic social defeat stress (CSDS) mice. Bullatine A can be used for the study of inflammation, glioblastoma (GBM) and depression .

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